Assay Detail
Binding
CHEMBL662472
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against radioligand [125I]CCK-8 binding to gastrin/Cholecystokinin type B receptor from rat brain
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL3508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 9.50 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | 2.0 | 1 | 10.00 |
| CHEMBL332024 | — | — | 1 | 9.96 |
| CHEMBL326102 | — | — | 1 | 9.96 |
| CHEMBL115121 | — | — | 1 | 9.96 |
| CHEMBL114277 | — | — | 1 | 9.96 |
| CHEMBL114072 | — | — | 1 | 9.85 |
| CHEMBL115833 | — | — | 1 | 9.80 |
| CHEMBL330933 | — | — | 1 | 9.77 |
| CHEMBL325863 | — | — | 1 | 9.70 |
| CHEMBL332931 | — | — | 1 | 9.68 |
| CHEMBL115612 | — | — | 1 | 9.37 |
| CHEMBL422604 | — | — | 1 | 9.36 |
| CHEMBL430516 | — | — | 1 | 9.30 |
| CHEMBL115772 | — | — | 1 | 9.28 |
| CHEMBL325746 | — | — | 1 | 9.23 |
| CHEMBL116300 | — | — | 1 | 9.08 |
| CHEMBL114991 | — | — | 1 | 8.90 |
| CHEMBL330917 | — | — | 1 | 8.89 |
| CHEMBL113988 | — | — | 1 | 8.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL332024 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL326102 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL115121 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL114277 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL114072 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL115833 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL330933 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL325863 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL332931 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL115612 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL422604 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL430516 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL115772 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL325746 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL116300 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL114991 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL330917 | — | IC50 | = | 1.29 | nM | 8.89 |
| CHEMBL113988 | — | IC50 | = | 3.29 | nM | 8.48 |